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| Title: | Imidazo[2,1-b]benzazepine derivatives, compositions and method of use |
| Abstract: | The present invention is concerned with novel imidazo[2, 1-b][3]benzazepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R.sup.1 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.3 represents hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; R.sup.4 represents hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, phenyl or halo; R.sup.5 represents hydrogen, C.sub.1-4 alkyl or halo; L represents hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyloxycarbonyl-C.sub.1-4 alkyloxy, hydroxycarbonylC.sub.1-4 alkyloxy, C.sub.1-4 alkyloxycarbonylamino, C.sub.1-4 alkylaminocarbonyl, C.sub.1-4 alkylaminocarbonylamino, C.sub.1-4 alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C.sub.1-6 alkyl substituted with both hydroxy and aryloxy; C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl; or, L represents a radical of formula --Alk--Y--Het.sup.1 (a-1),--Alk--NH--CO--Het.sup.2 (a-2)or --Alk--Het.sup.3 (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is ecxluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same. |
| Inventor(s): | Janssens; Frans E. (Bonheiden, BE), Diels; Gaston S. M. (Ravels, BE), Leenaerts; Joseph E. (Rijkevorsel, BE) |
| Assignee: | Janssen Pharmaceutica N.V. (Beerse, BE) |
| Application Number: | 08/142,474 |
| Patent Claim Types: see list of patent claims | Compound; Composition; Use; |
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | Type | RLD | Patent No. | Product | Substance | Delist_Flag | Patent Expiration | Patented / Exclusive Use | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Allergan | LASTACAFT | alcaftadine | SOLUTION/DROPS; OPHTHALMIC | 022134 | Jul 28, 2010 | RX | Yes | 5,468,743 | Y | Y | <disabled> | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| PCT Information | |||
| PCT Filed | June 09, 1992 | PCT Application Number: | PCT/EP92/01330 |
| PCT Publication Date: | December 23, 1992 | PCT Publication Number: | WO92/22551 |
| Country | Document Number | Publication Date | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Zambia | 2992 | May 25, 1994 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| South Africa | 9204326 | Dec 13, 1993 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| WIPO (PCT) | 9222551 | Dec 23, 1992 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Slovenia | 9200105 | Dec 31, 1992 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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